Phosphorous prodrugs and therapeutic delivery systems using same
AssigneeDrug Innovation & Design, Inc.
InventorArnold Glazier
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Abstract
The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells and into tissues in vivo. Prodrugs for a variety of antiviral and anti-leukemic agents are described.
Claims38
A prodrug compound for a parent drug, wherein the parent drug has the structure:
- ##STR31## wherein X is oxygen or sulfur;
- n is 1 or 2;
- and
- Y is defined by the remainder of the parent drug, with the proviso that the parent drug is not phosphoric acid;
- wherein the prodrug compound has the structure:
- ##STR32## wherein X, n and Y are defined above;
- and A is a benzyloxy derivative with one or more acyloxy groups in para or ortho positions relative to the phosphoester.
A prodrug compound for a phosphate or phosphonate bearing parent drug which is a mono or diester of the phosphate or phosphonate bearing parent drug wherein the prodrug is degraded to the parent phosphorous bearing drug by an elimination reaction to form a carbon-carbon double bond;
- and wherein the elimination reaction is triggered by the spontaneous or enzymatic unmasking of a strongly electron donating group.
Dependencies are inferred from the claim text.